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10074-G5 c-Myc inhibitor

Catalog No.C5722
Size Price Stock Qty
5mg
$62.00
In stock
10mg
$97.00
In stock
25mg
$179.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

10074-G5

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Chemical Properties

Cas No. 413611-93-5 SDF Download SDF
Chemical Name N-[1,1'-biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine
Canonical SMILES O=[N+](C(C1=NON=C12)=CC=C2NC3=CC=CC=C3C4=CC=CC=C4)[O-]
Formula C18H12N4O3 M.Wt 332.3
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

10074-G5 is a c-Myc inhibitor [1].

c-Myc is a bHLH-ZIP transcription factor involved in cell cycle progression, cellular growth and metabolism, differentiation, and apoptosis. Overexpression of c-Myc has been identified in numerous cancers, including prostate, pancreatic, lung, breast, and colon cancers, B-cell lymphoma, and leukemias. Alterations in c-Myc have been associated with cancer aggressiveness and poor treatment prognosis. Inhibition of c-Myc is an attractive pharmacological approach in the development of new anticancer treatments. Inactivation of c-Myc rapidly results in cell-cycle arrest, apoptosis, tumor vascular degeneration, redifferentiation of tumor cells, and ultimately tumor regression [1].

The IC50 values of 10074-G5 against Daudi cells and HL-60 cells were 15.6 ± 1.5 μM and 13.5 ± 2.1 μM, respectively. 10074-G5 (10 μM) inhibited c-Myc/Max dimerization and decreased total c-Myc protein expression. In C.B-17 SCID mice bearing Daudi xenografts, treatment with 10074-G5, (20 mg/kg i.v., for 10 consecutive days) significantly inhibited tumor growth with no effects on body weight.

References:
[1] Clausen D M, Guo J, Parise R A, et al.  In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization[J]. Journal of Pharmacology and Experimental Therapeutics, 2010, 335(3): 715-727.